SEW2871

Alias: SEW2871; SEW2871; SEW2871
Cat No.:V14699 Purity: ≥98%
SEW2871 (SEW-2871) is a S1P1 agonist (sphingosine-1-phosphate type 1 receptor agonist) with EC50 of 13.8 nM.
SEW2871 Chemical Structure CAS No.: 256414-75-2
Product category: LPL Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

SEW2871 (SEW-2871) is a S1P1 agonist (sphingosine-1-phosphate type 1 receptor agonist) with EC50 of 13.8 nM. SEW2871 enhances cognitive performance in rats modelled by Alzheimer's disease. SEW2871 increases the survival time of mice receiving heterotopic heart allografts. When it comes to the lysis of K562 tumor cells and dendritic cells mediated by natural killer cells, SEW2871 reverses the inhibitory effect of S1P, but not when it comes to cytokine release. SEW2871 increases the survival time of mice receiving heterotopic heart allografts. Diabetes, Alzheimer's, liver fibrosis, and inflammatory reactions are among the conditions for which it might be used.

Biological Activity I Assay Protocols (From Reference)
Targets
S1PR1 ( EC50 = 13.8 nM )
ln Vitro
SEW2871 shows enhanced migration effects by upregulating smooth muscle α-actin, procollagen αI and αIII, and total collagen content in LX-2 cells, a human hepatic stellate cell line [2].
ln Vivo
SEW2871 (20 mg/kg, gavage, once daily for 2 weeks) improves established experimental ductitis in IL-10–/– mice [3]. SEW2871 (0.5 mg/kg IP once daily) SEW2871 (0-0.3 mg/kg IV for 2 weeks) inhibits amyloid beta (Aβ1-42) in a trajectory model of Alzheimer's disease Induced spatial impairment memory and hippocampal neuron loss [2]. ) attenuates LPS-induced acute stress-induced lung injury in C57Bl/6 electrodes by producing the required alveolar and vascular septal protection [2]. SEW2871 reduces CD4+ T cell respiration inside the electrode and effectively protects cardiovascular short circuit animal models: IL-10–/– (interleukin (IL)-10 gene deficiency) mice, mouse model of Crohn’s disease (CD) [3] Dosage: 20 mg/kg Administration method: gavage. , once daily for 2 weeks Results: Colitis ameliorated in IL-10–/– mice, associated with reduced serum amyloid A concentration, reduced colonic MPO concentration, peripheral CD4+CD45+ T cell depletion, and T cell homing to colon LP. Inhibits typical cytokine and p-STAT-3 expression of type 1 helper T (Th1) and Th17 cells, and significantly reduces TNF-α, IFN-γ, IL-1β, and IL-17A mRNA levels.
Animal Protocol
IL-10–/– (interleukin (IL)-10 gene-deficient) mice, a murine model of Crohn's disease (CD)
20 mg/kg
Gavage, once daily for 2 weeks
References

[1]. Sphingosine 1-Phosphate Receptor Modulators and Drug Discovery. Biomol Ther (Seoul). 2017 Jan 1;25(1):80-90.

[2]. S1P1-selective in vivo-active agonists from high-throughput screening: off-the-shelf chemical probes of receptor interactions, signaling, and fate. Chem Biol. 2005 Jun;12(6):703-15.

[3]. Oral treatment with SEW2871, a sphingosine-1-phosphate type 1 receptor agonist, ameliorates experimental colitis in interleukin-10 gene deficient mice. Clin Exp Immunol. 2014 Jul;177(1):94-101.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H10F6N2OS
Molecular Weight
440.3616
Exact Mass
440.04
Elemental Analysis
C, 54.55; H, 2.29; F, 25.89; N, 6.36; O, 3.63; S, 7.28
CAS #
256414-75-2
Related CAS #
256414-75-2
Appearance
Solid powder
SMILES
C1=CC=C(C=C1)C2=C(SC(=C2)C3=NC(=NO3)C4=CC(=CC=C4)C(F)(F)F)C(F)(F)F
InChi Key
OYMNPJXKQVTQTR-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H10F6N2OS/c21-19(22,23)13-8-4-7-12(9-13)17-27-18(29-28-17)15-10-14(11-5-2-1-3-6-11)16(30-15)20(24,25)26/h1-10H
Chemical Name
5-[4-phenyl-5-(trifluoromethyl)thiophen-2-yl]-3-[3-(trifluoromethyl)phenyl]-1,2,4-oxadiazole
Synonyms
SEW2871; SEW2871; SEW2871
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~25 mg/mL (~56.8 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2709 mL 11.3543 mL 22.7087 mL
5 mM 0.4542 mL 2.2709 mL 4.5417 mL
10 mM 0.2271 mL 1.1354 mL 2.2709 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Change of colon lengths in mice treated with water or SEW2871. Clin Exp Immunol . 2014 Jul;177(1):94-101.
  • SEW2871 treatment ameliorated spontaneous colitis in IL-10–/– mice. Clin Exp Immunol . 2014 Jul;177(1):94-101.
  • Effect of SEW2871 on colonic proinflammatory cytokine mRNA expression using quantitative real-time–polymerase chain reaction (qRT–PCR) analysis. Clin Exp Immunol . 2014 Jul;177(1):94-101.
  • Both S1P and SEW2871 Induce Phosphorylation of ERK1/2 and Akt in CHO Cells Stably Transfected with S1P1. Chem Biol . 2005 Jun;12(6):703-15.
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